Details

Autor(en) / Beteiligte

• Biava, M
• Fioravanti, R
• Porretta, G C
• Frachey, G
• Mencarelli, P
• Sleiter, G
• Perazzi, M E
• Simonetti, N
• Villa, A

Titel

Study of the Mannich reaction: beta-amino-methylation of N-aryl and N-azaheteroaryl-substituted 2,5-dimethylpyrroles, compounds with potential biological activity

Ist Teil von

• Farmaco (Società chimica italiana : 1989), 1995-06, Vol.50 (6), p.431

Ort / Verlag

France

Erscheinungsjahr

1995

Quelle

MEDLINE

Beschreibungen/Notizen

• Owing to the increasing need of drugs for the treatment of a variety of fungal and bacterial opportunistic infections, a study has been started with the aim of synthesizing structures amenable to a number of easily-to-perform structural modifications in order to meet the requirement of bypassing resistance phenomena. This paper reports on the synthesis of several N-(alpha-azaheteroaryl)-substituted 2,5-dimethyl-pyrroles bearing in one beta-position (or in both beta-positions) aminomethyl groups, introduced via a Mannich reaction. Electronic and steric effects by the N-(azaheteroaryl) substituents and the 2- and 5-methyl groups on the course of the Mannich reaction are discussed along with the results of in vitro tests against many Candida species, some bacteria, and several pathogenic plant fungi.